2011 Fiscal Year Final Research Report
Clarification research for molecular mechanism of a novel type of protein kinase C inhibitor
| Project/Area Number |
21603016
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| Research Category |
Grant-in-Aid for Scientific Research (C)
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| Allocation Type | Single-year Grants |
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| Section | 一般 |
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| Research Field |
Chemical biology
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| Research Institution | The Institute of Physical and Chemical Research |
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Principal Investigator |
SODEOKA Mikiko 独立行政法人理化学研究所, 袖岡有機合成化学研究室, 主任研究員 (60192142)
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| Co-Investigator(Kenkyū-buntansha) |
HIRAI Go 独立行政法人理化学研究所, 袖岡有機合成化学研究室, 専任研究員 (50359551)
TAMURA Yuki 独立行政法人理化学研究所, 袖岡有機合成化学研究室, 客員研究員 (50442984)
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| Project Period (FY) |
2009 – 2011
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| Keywords | プロテインキナーゼC / 酵素阻害剤 / Isobenzofuranone誘導体 / ホスファチジルセリン / 構造活性相関 / 有機合成 |
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| Research Abstract |
In this research grant, we intended to clarify the activation mechanism of protein kinase C(PKC) at molecular level by utilizing isobenzofuranone(IB) derivatives, which were designed based on the physiological activators, diacylglycerols(DAG), for PKC. IB derivatives showed either activation or inhibition of PKC・depended on their substituents. Although the main subject of this research was clarification of the inhibition mechanism of PKC inhibitor IB-15A, analysis of the PKC activators was also necessary. In these three years, we first revealed the features of several PKC activators. And then we found that a potent PKC inhibitor IB-15A showed inhibition of PKC・by probably through the distinct binding site from that of the typical PKC activator and by disturbing the interaction of PKC with lipid.
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Research Products
(7 results)
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[Journal Article] Asymmetric synthesis of isobenzofuranone derivatives and their unique character as protein kinase Cα(PKCα) activators2009
Author(s)
Hirai, G., Ogoshi, Y., Ohkubo, M., Tamura, Y., Watanabe, T., Shimizu, T. and Sodeoka, M.
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Journal Title
Tetrahedron Lett
Volume: 50
Pages: 3609-3612
Peer Reviewed
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